Dorzolamide + Timolol - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

Dorzopt Plus

drops d / eye

ROMFARMA, OOO Russia

Kosopt

drops d / eye

Santen, AO Finland

АТХ:

S.01.E.X Other antiglaucoma drugs

Pharmacodynamics:

Combined drug, has anti-glaucoma effect. Each of the components lowers the intraocular pressure by decreasing the secretion of aqueous humor.

Dorzolamide - an inhibitor of carbonic anhydrase; reduces the secretion of intraocular fluid (slowing the formation of bicarbonate, followed by a decrease in the transfer of sodium and water). Does not cause a spasm of accommodation, miosis, gemeralopia.

Timolol - non-selective beta-blocker with negligible internal sympathomimetic activity. With topical application lowers the intraocular pressure by reducing the formation of watery moisture and a small increase in its outflow.

Pharmacokinetics:

Dorzolamide

It penetrates the eye mainly through the cornea (to a lesser extent through the sclera or limbus). Systemic absorption is low. After entering the blood quickly penetrates into the red blood cells containing a significant amount of carbonic anhydrase II. Binding to plasma proteins - 33%.

It is transformed into an N-desethylated metabolite,less active against carbonic anhydrase II, but capable of blocking carbonic anhydrase I. For long-term use, it accumulates in erythrocytes. It is excreted by the kidneys in the unmodified form and in the form of metabolites. After withdrawal, the rapid phase of withdrawal is replaced by a slow one, caused by the gradual release of dorzolamide from erythrocytes, with a half-life about 4 months.

Timolol

With topical application timolol penetrates into the systemic circulation. The concentration of timolol in plasma was studied in 6 patients with topical administration of timolol in the form of eye drops 0.5% 2 times a day. Average C_max after morning use was 0.46 ng / ml, after application in the afternoon - 0.35 ng / ml.

Indications:

Open angle (including secondary) glaucoma; pseudoexfoliation glaucoma; intraocular hypertension.

ICD-10

VII.H40-H42.H40.5 Glaucoma secondary due to other eye diseases

VII.H40-H42.H40.4 Glaucoma secondary due to inflammatory disease of the eye

VII.H40-H42.H40.3 Glaucoma secondary posttraumatic

VII.H40-H42.H40.1 Primary open angle glaucoma

Contraindications:

Hypersensitivity, bronchial asthma, bronchospasm, bradycardia,AV-block II-III level, chronic heart failure II-III degree, cardiogenic shock, chronic renal failure (creatinine clearance less than 30 mL / min).

Carefully:

Hepatic insufficiency, child and elderly age.

Before starting the use of the drug, it is necessary to provide adequate control of the state of the cardiovascular system. Patients with a history of severe cardiac disease and signs of heart failure should be closely monitored.

Caution is prescribed to patients with diabetes mellitus, since beta-blockers may mask the symptoms of acute hypoglycemia.

Pregnancy and lactation:

Recommendations FDA category C. Adequate controlled studies in humans have not been conducted. Do not apply!

In the rat studies have shown that the use of timolol at a dose of 50 mg / kg per day, causes a delay of ossification fetus. Side effects that affect the postnatal development of offspring are not documented. In studies on rabbits and mice teratogenic effects have not been established. Dorzolamide in rodents causes limb defects in fruits.

Penetrates into breast milk when absorbing an ophthalmic solution. Do not apply.

Dosing and Administration:

Bury 1 drop in the conjunctival sac 2 times a day. If several local ophthalmic drugs are used in the treatment, the administration of medication should be done at an interval of 10 minutes.

Side effects:

Dorzolamide: burning, paresthesia, itching in the eyes, lacrimation, blurred vision, eyelid irritation, superficial pinpoint keratitis, conjunctivitis, myopia, blepharitis; rarely - iridocyclitis. Allergic reactions, bitterness in the mouth, nausea, headache, asthenia.

Timolol: hyperemia of the conjunctiva, lacrimation, photophobia, corneal epithelial edema, burning and itching in the eyes, hyperemia of the eyelid skin, diplopia, blepharitis, keratitis, decreased corneal sensitivity, ptosis. With prolonged use in high doses, systemic side effects are possible.

Overdose:

Symptoms of unintentional thymolol overdose in the form of eye drops with the development of systemic effects of beta-adrenoblocker overdose for systemic use: dizziness, headache, dyspnea, bradycardia, bronchospasm, cardiac arrest.

The most anticipated symptoms of an overdose of dorzolamide are a violation of the electrolyte balance, the development of acidosis, headache, asthenia / fatigue, paresthesia.

Treatment: conduct symptomatic and supportive therapy. The concentration of electrolytes (primarily sodium) and the pH of the blood plasma should be monitored. In studies it is also shown that timolol not output during dialysis.

Interaction:

Antiglaucoma drugs (beta-blockers, pilocarpine, dipyvephrine, carbachole) intensify the action. With simultaneous use of inhibitors of carbonic anhydrase and beta-adrenoblockers, an additive effect on systemic effects is possible.

Timolol enhances the action of muscle relaxants and general anesthetics.

Special instructions:

During the treatment period, it is necessary to regularly measure intraocular pressure, monitor the function of tearing, the integrity of the cornea, the visual field - at least once every 6 months.

With prolonged therapy, it is necessary to control the potassium concentration, electrolytes in blood serum, blood pH, heart rate, blood pressure and other parameters of cardiac activity.

Care must be taken when driving a car at night, restricting activity in poor lighting.

The drug can be used by patients who use hard contact lenses made of polymethylmethacrylate. The preservative contained in the preparation can be deposited on soft contact lenses, so the lens should be removed before instillation and put on not earlier than 15 minutes after it.

In the case of an upcoming surgical intervention with general anesthesia, it is necessary to cancel the drug 48 hours before surgery, since timolol strengthens the action of muscle relaxants and general anesthetics.

Instructions

Dorzolamide + Timolol (Dorzolamidum + Timololum)